کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360766 | 981447 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Axial chirality and affinity at the GABAA receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The pyrimido[1,2-a][1,4]benzodiazepines (1a–c) and the 8-membered analogues (diazocines 2a and 2b) were separated into their atropisomers with HPLC on a chiral column. High stereochemical stability was observed in the atropisomer of the 8-membered derivatives (2a and 2b), and the 1,4-benzodiazepine (1c) with 2′-chloro at the pendant phenyl showed a lower energy barrier for the conversion between the atropisomers compared with that with the unsubstituted pendant phenyl (1a). The aR isomer of 1a–c was revealed to be the eutomer in GABAA receptor binding, and the eutomer 1c-R showed extremely potent activity with an IC50 value of 1.5 nM.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 21, 1 November 2008, Pages 9519–9523
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 21, 1 November 2008, Pages 9519–9523
نویسندگان
Shoukou Lee, Tomonori Kamide, Hidetsugu Tabata, Hideyo Takahashi, Motoo Shiro, Hideaki Natsugari,